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Assay Detail

CHEMBL3294387

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Competitive inhibition of EZH2 histone methyltransferase activity in EZH2/SUZ12/EED/RbAp46/48 (unknown origin) using histone H3 peptide/varying concentration of S-adenosylmethionine as substrate after 2 hrs by Lineweaver-Burk plot analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

EZH2/SUZ12/EED/RBBP7/RBBP4 (CHEMBL3301388)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Biological evaluation of tanshindiols as EZH2 histone methyltransferase inhibitors.
Woo J, Kim HY, Byun BJ, Chae CH, Lee JY, Ryu SY, Park WK, Cho H, Choi G.
Bioorg Med Chem Lett (2014) 24 : 2486 -2492
PubMed 24767850 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 6.71 6.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3287734 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3287734 Ki = 194.0 nM 6.71